Assay Detail
Binding
CHEMBL4012830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant rat GluN1/GluN2D receptor expressed in xenopus laevis oocyte assessed as potentiation of glutamate and glycine-induced current response at holding potential -40mV by two electrode voltage clamp method
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Ionotropic glutamate receptor NMDA 1/2D (CHEMBL3038506) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
The Structure-Activity Relationship of a Tetrahydroisoquinoline Class of N-Methyl-d-Aspartate Receptor Modulators that Potentiates GluN2B-Containing N-Methyl-d-Aspartate Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 44 | 5.70 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4061206 | — | — | 1 | 6.55 |
| CHEMBL4100452 | — | — | 1 | 6.48 |
| CHEMBL4091770 | — | — | 1 | 6.39 |
| CHEMBL4063861 | — | — | 1 | 6.37 |
| CHEMBL4070902 | — | — | 1 | 6.36 |
| CHEMBL4099510 | — | — | 1 | 6.35 |
| CHEMBL4064008 | — | — | 1 | 6.32 |
| CHEMBL4083076 | — | — | 1 | 6.24 |
| CHEMBL2397256 | — | — | 1 | 6.00 |
| CHEMBL4091772 | — | — | 1 | 6.00 |
| CHEMBL4091645 | — | — | 1 | 5.96 |
| CHEMBL4062279 | — | — | 1 | 5.92 |
| CHEMBL4081483 | — | — | 1 | 5.92 |
| CHEMBL4068612 | — | — | 1 | 5.85 |
| CHEMBL4099073 | — | — | 1 | 5.82 |
| CHEMBL4089357 | — | — | 1 | 5.80 |
| CHEMBL4064435 | — | — | 1 | 5.80 |
| CHEMBL4064895 | — | — | 1 | 5.77 |
| CHEMBL4069391 | — | — | 1 | 5.77 |
| CHEMBL4096621 | — | — | 1 | 5.72 |
| CHEMBL4101985 | — | — | 1 | 5.70 |
| CHEMBL4100185 | — | — | 1 | 5.66 |
| CHEMBL4066872 | — | — | 1 | 5.58 |
| CHEMBL4073018 | — | — | 1 | 5.57 |
| CHEMBL4061988 | — | — | 1 | 5.54 |
| CHEMBL4095932 | — | — | 1 | 5.52 |
| CHEMBL4083829 | — | — | 1 | 5.52 |
| CHEMBL4072003 | — | — | 1 | 5.47 |
| CHEMBL4093717 | — | — | 1 | 5.47 |
| CHEMBL4088927 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4061206 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4100452 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4091770 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4063861 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4070902 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4099510 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4064008 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4083076 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2397256 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4091772 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4091645 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4081483 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4062279 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4068612 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4099073 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4089357 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4064435 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4064895 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4069391 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4096621 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4101985 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4100185 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4066872 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4073018 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4061988 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4095932 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4083829 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4072003 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4093717 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4088927 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4073626 | — | EC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4103457 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4073306 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4101865 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4064718 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4081036 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4060709 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4078507 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4085532 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4102790 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4085970 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4102354 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4093976 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4073331 | — | EC50 | - | — | - |